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The study of drugs in humans is referred to as
Clinical pharmacology
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The study of drugs and their interactions with living systems is the definition of
Pharmacology
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Therapeutic or pharmacotherapeutics is defined as
the use of drugs to diagnose, prevent, or treat disease or to prevent pregnancy
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Any chemical that can affect living processes is a
Drug
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the three most important characteristics that anyt drug can have are
- effectiveness
- safety
- selectivity
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The Greek word pharmakon is translated as
Poison
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Some drugs interact with one another. The antibacterial effects of tetracycline can be greatly reduced by taking??
iron or calcium supplements
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The objective of drug therapy is to provide
maximum benefit with minimum harm
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The four major pharmacokinetic processes are
- drug absorption
- drug distribution
- drug metabolism
- drug excretion
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Pharmacodynamics may be thought of as
the impact of drugs on the body
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What are the five rights of drug administration
- right drug
- right patient
- right dose
- right route
- right time
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Who is the most likely member of the health care team to observe and evaluate drug responses and to intervene if required??
The Nurse
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the three basic goals of preadministration assessment of medications are
Collecting baseline data needed to evaluate therapeutic and adverse responses, identifying high risk patients, assessing the patients capacity for self care
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Important predisposing factors in identifying high risk patients are
- pathophysiology
- genetic factors
- drug allergies
- pregnancy
- old age
- extreme youth
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Certain drugs have more thaqn one indication, and the dosage may differ depending on the indication for which the drug is used. Aspirin is given in low doses to
relieve pain and in high doses to suppress inflammation
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Measures to reduce adverse effects of medication administration include
- identifying high risk patients through the patient history
- ensuring proper administration through patient education
- forewarning patients about activities that might precipitate an adverse reaction
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Patients taking insulin therapy should be taught that early signs of hypoglycemia include
sweating and increased heart rate
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Contraindication (or Precaution)
a pre-existing condition that significantly increases the risk of an adverse reaction to a particular drug, but not to a degree that is life threatening
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Among geriatric patients, the most common cause of failed self medication is
Conviction that the drug simply was not needed in the dosage prescribed
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A harmless side effect of rifampin is
red-orange color to urine
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the first legislation to regulate drug safety passed in 1938 was the
Food, Drug and Cosmetic Act
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This law was created in response to the thalidomide tragedy that occurred in Europe in the early 1960's
Harris-Kefauver Amendments
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the first American law to regulate drugs was the
Federal Pure Food and Drug Act of 1906
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In the early 1960's thalidomide was widely used by pregnant women, and thousands of infants were born with ???
Phocomelia
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Phocomelia
a rare birth defect characterized by the gross malformation or complete absence or arms or legs
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Under conditions of the controlled substance Act, schedule I drugs
Have no medical use in the United States and are deemed to have a high potential for abuse
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In the United States, the estimated cost of developing a new drug can exceed
800 million dollars
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Randomized controlled trials are
the most reliable way to objectively assess drug therapies
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Phase I drugtrials are usually conducted in
normal volunteers
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Phase II and Phase III trials are tested in
Patients
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The chemical name constitutes
a description of a drug using the nomenclature of chemistry
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The Generic name
is assigned by the U.S. Adopted Names Council
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The Trade name, Proprietary name, and Brand names are names
under which a drug is marketed
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Drugs that can be purchased without a prescription are referred to as
Over the counter drugs
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Pharmacokinetics
The study of drug movement through the body
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In order for a drug to directly penetrate membranes, it must be
Lipid soluble
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Factors that affect drug absorption iclude
- rate of dissolution
- surface area
- blood flow
- lipid solubility
- pH partitioning
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Enteric-coated preparations
consist of drugs that have been covered with a material designed to dissolve in the intestine but not the stomach
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Most dug metabolism take place in the
liver
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Nonrenal routes of drug excretion include
- breast milk
- bile
- enterohepatic recirculation
- lungs
- sweat
- saliva
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Three procedures that can be employed to reduce fluctuations in drug levels are
- Continuous infusion
- administration of a depot preparation
- reduction of both the dosage size and dosing interval
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The therapeutic range of a drug lies between the
minimum effective concentration and toxic concentration
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Most drugs are excreted by the
Kidneys
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Oral administration of medications has the advantages of
- Ease
- convenience
- inexpensive
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Pharmacodynamics
the study of the biochemical and physiologic effects of drugs and the molecular mechanisms by which those effects are produced
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The greatest effect a drug can produce is called the
maximal efficacy
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Potency
refers to the amount of drug we must give to elicit and effect
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A Receptor
any functional macromolecule in a cell to which a drug binds to produce its effects.
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The function of the transcription factors is to
regulate protein synthesis
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The modified theory ascribes two qualities to drugs
Affinity and intrinsic activity
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Affinity refers to the
Strength of the attraction between a drug and its receptor
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And intrinsic activity refers to
the ability of a drug to activate a receptor upon binding
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Drugs that mimic the body's regulatory molecules are called
Agonists
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Drugs that block the actions of endogenous regulators are called
Antagonists
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When the receptors of a cell are continually exposed to an agonist, the cell usually becomes less responsive, the cell is said to be
desensitized or refractory or to have undergone down- regulation
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The four primary families of receptors are
- cell membrane-embedded enzymes
- ligand-gated ion channels
- G protein-coupled receptor systems
- transcription factors
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The therapeutic index is defined as
the ratio of a drug's LD50 to its ED50
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Patients receiving both halothane and succinylcholine may develop
malignant hyperthermia
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Three possible outcomes that may occur when drug A interacts with Drug B are:
- Drug A may intensify the effects of drug B
- Drug A may reduce the effects of drug B
- the combination of drug A and drug B may produce a new response no seen with either drug alone
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When a patient is taking two medications and one drug may intensify the effects of the other, the interaction is termed
Potentiative
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Interactions that result in reduced drug effects are often termed
Inhibitory
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Direct interactions are most commonly found when drugs are combined
in IV solutions
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Interactions are especially important for drugs that have a
low therapeutic index
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Some foods cause decreased absorption of drugs. Absorption of digoxin is significantly reduced by
- Wheat bran
- Rolled oats
- Sun flower seeds
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The most dramatic example of drug-food interactions that sometimes increase toxicity is the interaction between
- Monoamine oxidase inhibitors (a family of antidepressants),
- Foods rich in tyramine (aged cheese, yeast extracts, Chianti)
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Any noxious, unintended, and undesired effect that occurs at normal drug doses is defined by the World Health Organization as an
Adverse drug reaction
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Mild adverse drug reactions include
- Drowsiness
- nausea
- itching
- rash
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Severe reactions include
- respiratory depression
- neutropenia
- hepatocellular injury
- anaphylaxis
- hemorrhage
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Mide adverse and Severe reactions can both result in
Death
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A side effect is formally defined as
A nearly unavoidable secondary drug effect produced at therapeutic doses
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Toxicity
an adverse drug reaction caused by excessive dosing
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Mos serious reactions are caused by one group of drugs
Penicillins
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Other drugs are noted for causing allergic reactions including the
sulfonamide group of compounds
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An uncommon drug response resulting from a genetic predisposition is called an
idiosyncratic effect
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A disease caused by a drug is called an
iatrogenic disease
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A state in which the body has adapted to prolonged drug exposure in such a way that an abstinence syndrome will result if drug use is discontinued is known as
Physical dependence
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Drug-induced birth defects are referred to as
teratogenic effects
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The patient's last line of defense against medication errors made by others is the
Nurse
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Dosage adjustments based on adverse drug reaction provide
more precise means of controlling drug responses than do adjustments based on weight alone
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Drug sensitivity varies with age. In infants
heightened drug sensitivity is the result of organ immaturity
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In the Elderly, heightened sensitivity results largely from
organ degeneration
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Why do we not know much about gender-related differences in drug therapy
because until recently, essentially all drug research was done in men
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Perhaps the most important example of an altered drug effect occurring in response to electrolyte imbalance involves digoxin and
Potassium
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Decreased responsiveness to a drug, as a result or repeated drug administration is called
tolerance
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The type of tolerance associated with long-term administration of drugs such as morphine and heroin is
pharmocodynamic tolerance
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A form of tolerance that can be defined as a reduction in drug responsiveness brought on by repeated dosing over a short time is called
Tachyphylaxis
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Placebo effect
a component of a drug response that is caused by psychologic factors and not by the biochemical or physiologic properties of the drug
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Bioavailability
refers to the ability of a drug to reach the systemic circulation from its site of administration
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Some factors that influence patient compliance include
- manual dexterity
- visual acuity
- intellectual capacity
- psychologic state
- attitude toward drugs
- the ability to pay for medications
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By the third trimester, renal blood flow in the pregnant woman has
Doubled
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Is it true that drugs taken by the mother do no cross the placenta??
No; any drug taken during pregnancy will reach the fetus
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Teratogensis
the production of birth defects
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symptoms of withdrawal syndrome in the infant include
- shrill crying
- vomiting
- extreme irritability
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Down's syndrome
of the genetically based anomalies is it is the most common
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Gross malformations are produced by exposure to teratogens during the
Embryonic period
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Teratogen exposure during the
Fetal period; usually disrupts the function rather than gross anatomy
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The teratogen Diethylstilbestrol is an
estrogenic substance that causes vaginal cancer in female offspring 18 o so years after birth
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An example of a functional impairment that results from exposure to teratogen later in pregnancy is
Mental retardation
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Drug sensitivity in the very young results largely from
Organ system immaturity
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Drug sensitivity in the elderly results largely from
Organ system degeneration
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The pediatric age group includes all patients younger than
16 years of age
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Premature infants
Less than 36 weeks gestational age
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Full-term infants
36-40 weeks gestational age
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neonates
first 4 postnatal weeks
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infants
weeks 5 to 52 postnatal
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adolescents
12 to 16 years
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how do drugs affect the blood-brain barrier of the infant?
because the blood-brain barrier is not fully developed at birth, drugs and other chemicals have relatively easy access to the central nervous system, making the infant especially sensitive to drugs that affect the CNS.
All medications employed for their CNS effects should be given in reduced dosages
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Complete maturation of the liver is accomplished by age
1 year
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Adult levels of renal function are achieved by age
1 year
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In the pediatric population, adverse drug reactions to fluoroquinolones may cause
tendon rupture
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Adverse drug reactions to nalidxic acid may cause
cartilage erosion
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Children 1 to 12 years of age differ pharmacokinetically from adults in that children metabolize drugs
Faster
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The method of conversion of adult dosages of drugs to pediatric dosages of drugs employed most commonly is based on
Body surface area
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The four major factors that can alter drug distribution in the elderly include
- Increased percentage of body fat
- decreased percentage of lean body mass
- decreased total body water
- reduced concentration of serum albumin
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The most important cause of adverse drug reactions in the elderly is
drug accumulation secondary to reduced renal excretion
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In the elderly the proper index of renal function is
Creatinine clearance
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Factors underlying the increase in adverse reactions in the geriatric population include
- polypharmacy
- severe illness
- multiple pathologies
- treatment with dangerous drugs
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Neuropharmacology
the study of drugs that alter processes controlled by the nervous system
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Most neuropharmacologic agents act by altering
Synaptic transmission
only a few alter axonal conduction
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What are the only drugs that are proven to work by altering or decreasing axonal conduction??
Local anesthetics
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A drug with effects that mimic the effects of a natural transmitter would be said to
increase receptor activation
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A drug with effects that are equivalent to reducing the amount of natural transmitter available for receptor binding would be said to
Decrease receptor activation
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What is the effect of botulinum toxin
Botulinum toxin blocks the release of acetylcholine from the neurons that control skeletal muscles, including the muscles of respiration
Loss of function of the respiratory muscles and suffocation occur
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The most prominent responses to activation of beta 1 receptors are
increased heart rate and increased force of cardiac contraction
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The primary responses to activation of beta 2 receptors are
Bronchial dilation and elevation of glucose levels in the blood
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Drugs that increase receptor activation are called
Agonist drugs
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Drugs that decrease receptor activation are called
Antagonist drugs
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When you study each drug that has an effect on the peripheral nervous system you should learn
the identity of the receptors at which the drug acts
the normal responses to activation of those receptors
whether the drug increases or decreases receptor activation
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The peripheral nervous system has two major subdivisions
Somatic motor system
Autonomic nervous system
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The autonomic nervous system has three principal functions
- Regulation of the heart
- Regulation of the secretory glands
- Regulation of smooth muscle
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By influencing the heart and blood vessels, the sympathetic nervous system can achieve three homeostatic objectives
- 1. Maintenance of blood flow to the brain
- 2. Redistribution of blood flow during exercise
- 3. Compensation for loss of blood, primarily causing vasoconstriction
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From a pharmacologic perspective, the most important feedback loop of the autonomic nervous system is one that helps regulate blood pressure. It is referred to as the
Baroreceptor reflex
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The three neurotransmitters employed by the peripheral nervous system are
- Acetylcholine
- Norepinephrine
- Epinephrine
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Activation of nicotinic (muscle) causes
Contraction of skeletal muscle
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Activation of alpa receptors in the blood vessels produces
Vasoconstriction
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The release of renin promotes
Synthesis of angiotensin, a powerful vasoconstrictor;
Activation of renal beta1 receptors is a means by which the nervous system helps elevate blood pressure
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Epinephrine is released from the
Adrenal medulla
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Epinephrine's function is to
initiate the fight or flight response
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Activation of beta 1 receptors
- Increase the heart rate
- Increase the force of myocardial contraction
- Increases conduction through the Av node (promotes release of renin by the kidney)
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